ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

FIELD: medicine, pharmaceutics. SUBSTANCE: invention relates to novel compounds of general formula (1), which possess affinity for µ-opioid receptor and ORL1-receptor, to medications, containing said compounds, and to application of said compounds for obtaining medications, suitable for treating pain, fear, stress and other diseases or conditions. In general formula (1) Y 1 , Y 1 ', Y 2 , Y 2 ', Y 3 , Y 3 ', Y 4 and Y 4 ' stand for -H; R 1 and R 2 independently on each other stand for -H or -CH 3 ; on condition that R 1 and R 2 both simultaneously do not stand for -H; Q stands for: -C 6-16 -aryl, non-substituted or mono- or poly-substituted with -F, -Cl, -Br or -I; or heteroaryl; R 3 stands for: -C 1-8 -alkyl, non-substituted or mono- or poly-substituted -OR 0 , where R 0 stands for non-substituted -C 1-3 -alkyl; non-substituted -C 3-6 -cycloalkyl-C 1-4 -alkyl; non-substituted -C 1-4 -alkyl-C 3-6 -cycloalkyl; -C 6-16 -aryl, non-substituted or mono- or poly-substituted with -F, -Cl, -Br, -I, -CN, -R 0 or -OR 0 , where R 0 stands for non-substituted -C 1-8 -alkyl; or heteroaryl; n stands for 0; X stands for -NR A -; R A stands for -H or -R 0 ; where R 0 stands for non-substituted -C 1-4 -alkyl; and R B stands for -C(=O)R 0 ; where R 0 stands for non-substituted -C 2-8 -alkenyl-C 6-16 -aryl or non-substituted -C 1-8 -alkyl-(C 6-16 -aryl) 1-2 . EFFECT: obtaining compounds for obtaining medications, suitable for treatment of pain, fear, stress and other diseases or conditions. 10 cl, 14 tbl, 164 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 209/12 C07D 209/14 C07D 401/04 C07D 251/48 C07D 251/54 C07C 211/40 ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 233/36 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 233/46 C07C 311/18 C07D 211/62 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 525 236 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D A61K A61K A61K A61P A61P 213/12 213/82 309/08 31/137 31/404 31/53 25/00 9/00 C2 (2006.01 ...

ZNS EFFECTIVE 8-HETEROCYCLYL-2-AMINOTETRALIN of DERIVATIVES

Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide

Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5- tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

THERAPEUTICALLY USEFUL 2-AMINOTETRALIN DERIVATIVES

This invention is therapeutically useful 2-aminotetralins and pharmaceutical ly acceptable acid addition salts thereof of for- mula (I). These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Therapeutically useful 2-aminotetralin derivatives

치료학적으로 유용한 2-아미노테트랄린 유도체 Therapeutic Useful 2-Aminotetraline Derivatives 본 발명은 하기 일반식(I)의 치료학적으로 유용한 2-아미노테트랄린 및 그의 약학적으로 허용가능한 산 부가염에 관한 것이다 : The present invention relates to the therapeutically useful 2-aminotetraline of formula (I) and pharmaceutically acceptable acid addition salts thereof: 상기식에서, R, R 1 , R 2 , R 3 , R 4 , R 5 및 p는 상기 정의한 바와 같다. Wherein R, R 1 , R 2 , R 3 , R 4 , R 5 and p are as defined above. 상기 화합물은 중추신경계 질환, 고혈압증, 당뇨병, 성기능부전을 치료하고 식욕을 조절하는데 유용하다. The compound is useful for treating central nervous system disease, hypertension, diabetes, sexual dysfunction and controlling appetite.

置換された４−アミノシクロヘキサン誘導体

Patent RU2017131862A3

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

... 1. Соединение общей формулы (1)гдеY, Y', Y, Y', Y, Y', Yи Y' в каждом случае независимо друг от друга выбраны из группы, состоящей из -Н, -F, -Cl, -Br, -I, -CN, -NO, -CHO, -R, -C(=O)R, -C(=O)H, -C(=O)-OH, -C(=O)OR, -C(=O)NH, -C(=O)NHR, C(=O)N(R), -ОН, -OR, -OC(=O)H, -OC(=O)R, -OC(=O)OR, -OC(=O)NHR, -OC(=O)N(R), -SH, -SR, -SOH, -S(=O)-R, -S(=O)NH, -NH, -NHR, N(R), -N(R), -N(R)O, -NHC(=O)R, -NHC(=O)OR, -NHC(=O)NH, NHC(=O)NHRи -NHC(=O)N(R); преимущественно в каждом случае независимо друг от друга выбраны из группы, состоящей из -Н, -F, -Cl, -CN и -С-алифат; или Yи Y', или Yи Y', или Yи Y', или Yи Y' совместно означают =O;Q означает -R, -C(=O)-R, -C(=O)OR, -C(=O)NHR, -C(=O)N(R)или -C(=NH)-R;Rв каждом случае независимо означает -C-алифат, -С-циклоалифат, -арил, -гетероарил, -С-алифат-С-циклоалифат, -C-алифат-арил, -C-алифат-гетероарил, -С-циклоалифат-С-алифат, -С-циклоалифат-арил или -С-циклоалифат-гетероарил;Rи R, независимо друг от друга означают -Н или -R; или Rи Rсовместно образуют кольцо ...

ASCOCHLORIN DERIVATIVE AND USE THEREOF AS AMPK ACTIVATOR

An object of the present invention is to provide a novel ascochlorin derivative which activates adenosine monophosphate-activated protein kinase (AMPK), and is useful in the treatment or prevention of diseases or conditions that involve AMPK dysregulation. The present invention provides a compound presented by formula I, a pharmaceutically acceptable salt or a solvate thereof.

CYCLIC HYDROCARBON COMPOUND

Provided is a novel compound having an excellent suppression action against arrhythmia including atrial fibrillation and being useful as a pharmaceutical product having a separated antiviral effect. A compound indicated by general formula (I), a pharmacologically acceptable salt thereof, or a solvate of these (in the formula, the dotted line indicates a single bond and double bonds, R1 indicates a C1-6 alkyl group that may have a substituent, Q indicates an oxygen atom, a sulfur atom, or NR5, R2 indicates -(C=0)-R6, -CHR6R7, or -CH2OR8, and R3 and R4 are the same or different and indicate an amino group, an azide group, or -X-R9, provided that least either R3 or R4 is an amino group.) ...

Substituted 4-aminocyclohexane derivatives

2-AMINOINDANS AS SELECTIVE DOPAMINE D3 LIGANDS

Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of formula (I), wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CF3, CN, SR5, SO2NH2, SO2NR5R6, SO2R5, -OCO-C1-C6 alkyl, -NCO-C1-C6 alkyl, -CH2O-C1-C6 alkyl, -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-C1-C6 alkyl, phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazol, halogen (Br, Cl, F, I), R6 or R1 and R2 together form -O(CH2)mO- (where m is 1-2) or -CH2(CH2)pCH2 - (where p is 1-4); (except that only one of R1 and R2 can be hydrogen, OCH3 or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p-thienyl (where p is 1-4), hydrogen (except that only one of R3 and R4 can be hydrogen in any such compound) or C1-C8 alkyl (except where R1 or R2 are hydrogen, OCH3 or OH); R5 is hydrogen, C1-C8 ...

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds that have an affinity to the -opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

ЦИКЛИЧЕСКОЕ УГЛЕВОДОРОДНОЕ СОЕДИНЕНИЕ

FIELD: chemistry.SUBSTANCE: invention relates to a compound represented by the following general formula (I), or a pharmaceutically acceptable salt thereof, and a medicament and a pharmaceutical composition comprising the claimed compound or a pharmaceutically acceptable salt thereof, as well as to the use of the claimed compound or its pharmaceutically acceptable salt.(I). In the formula (I) dotted line indicates a single bond or double bond, Q represents an oxygen atom, a sulfur atom or NR, and R-Rhave the meaning given in the claims.EFFECT: compounds can be used to treat arrhythmias.10 cl, 2 tbl, 50 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 233/41 (2006.01) C07C 233/79 (2006.01) C07C 247/14 (2006.01) C07C 271/24 (2006.01) C07D 207/335 (2006.01) C07D 277/28 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 307/52 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 333/20 (2006.01) A61K 31/165 (2006.01) A61K 31/166 (2006.01) (12) (13) 2 676 328 C2 A61K 31/27 (2006.01) A61K 31/341 (2006.01) A61K 31/381 (2006.01) A61K 31/40 (2006.01) A61K 31/426 (2006.01) A61K 31/655 (2006.01) A61P 9/06 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК (21)(22) Заявка: 2016136493, 13.02.2015 (24) Дата начала отсчета срока действия патента: (73) Патентообладатель(и): ТОА ЭЙО ЛТД. (JP) Дата регистрации: 28.12.2018 (56) Список документов, цитированных в отчете о поиске: WO 2012147902 A1, 01.11.2012. A. Приоритет(ы): (30) Конвенционный приоритет: 14.02.2014 JP 2014-026617 (43) Дата публикации заявки: 19.03.2018 Бюл. № (45) Опубликовано: 28.12.2018 Бюл. № 1 2 6 7 6 3 2 8 (86) Заявка PCT: R U (85) Дата начала рассмотрения заявки PCT на национальной фазе: 14.09.2016 (54) ЦИКЛИЧЕСКОЕ УГЛЕВОДОРОДНОЕ СОЕДИНЕНИЕ (57) Реферат: Изобретение относится к соединению, заявленное соединение или его фармацевтически представленному следующей общей формулой приемлемую соль, а также к применению (I), или к его фармацевтически приемлемой соли, заявленного соединения или его фармацевтически которые могут быть ...

КРИСТАЛЛИЧЕСКИЕ ФОРМЫ (S)-5-БЕНЗИЛ-N-(5-МЕТИЛ-4-ОКСО-2,3,4,5-ТЕТРАГИДРОБЕНЗО[b][1,4]ОКСАЗЕПИН-3-ИЛ)-4H-1,2,4-ТРИАЗОЛ-3-КАРБОКСАМИДА

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

... 1. Соединение общей формулы (1)где Y, Y', Y, Y', Y, Y', Yи Y' означают -H;Q означает -арил или -гетероарил;Rи R, независимо друг от друга означают -Н или -СН; при условии, что Rи Rоба одновременно не означают -Н;Rозначает -C-алифат, -С-циклоалифат, -арил, -гетероарил, -C-алифат-С-циклоалифат, -С-алифат-арил, -C-алифат-гетероарил, -С-циклоалифат-С-алифат, -С-циклоалифат-арил или -С-циклоалифат-гетероарил;n означает 0;X означает -NR-;Rозначает -Н или -R; где Rозначает -C-алифат, -С-циклоалифат, -арил, -гетероарил, -C-алифат-С-циклоалифат, -С-алифат-арил, -С-алифат-гетероарил, -С-циклоалифат-C-алифат, -С-циклоалифат-арил или -С-циклоалифат-гетероарил;Rозначает -C(=O)R; где Rозначает -С-алифат-арил или -C-алифат-гетероарил;причем "алифат" в каждом случае представляет собой разветвленный или неразветвленный, насыщенный или моно- или многократно ненасыщенный, незамещенный или моно- или многократно замещенный, алифатический углеводородный остаток;"циклоалифат" в каждом случае представляет собой ...

2-AMINOINDANE AS SELECTIVE DOPAMIN-D3-LIGANDEN

compostos derivados substituídos de 4-aminociclohexano, medicamentos contendo pelo menos um composto e uso dos referidos compostos

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

FIELD: chemistry. SUBSTANCE: invention relates to novel compounds of general formula (1), which possess an affinity to the µ-opiod receptor and the ORL1-receptor. The invention also relates to the application of the said compounds for obtaining medications, which can be used in treatment of fear, stress and associated with stress syndromes, depressions, epilepsy, Alzheimer's disease, senile dementia, general cognitive dysfunctions, learning and memory disorders (as nootropic), withdrawal syndromes, alcohol and/or drug abuse and/or abuse of medications and/or alcohol, narcotic and medication addiction, etc. In general formula (1) (1) Y 1 , Y 1   ' , Y 2 , Y 2   ' , Y 3 , Y 3   ' , Y 4 and Y 4   ' in each case stand for -H; Q stands for -R 0 , -C(=O)-R 0 , -C(=O)OR 0 , -C(=O)NHR 0 , -C(=O)N(R 0 ) 2 or-C(=NH)-R 0 ; R 0 in each case stands for -C 1-8 -aliphate, -C 3-12 -cycloaliphate, -aryl, -heteroaryl, -C 1-8 -aliphate-C 3-12 -cycloaliphate, -C 1-8 -aliphate-aryl, -C 1-8 -aliphate-heteroaryl, -C 3-8 -cycloaliphate-C 1-8 -aliphate, -C 3-8 -cycloaliphate-aryl or -C 3-8 -cycloaliphate-heteroaryl; R 1 and R 2 independently on each other stand for -C- 1-8 -aliphate; R 3 stands for -C 1-8 -aliphate, -aryl, -heteroaryl or -C 1-8 -aliphate-C 3-12 -cycloaliphate; n stands for 0; X stands for -NR A -;R A stands for -C 1-8 -aliphate; R B stands for -C 1-8 -aliphate; on condition that R 1 , R 2 , R A and R B simultaneously do not stand for the non-substituted-C 1-8 -aliphate. EFFECT: increased efficiency of the application of the compounds. 9 cl, 11 tbl, 164 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 209/12 C07D 209/14 C07D 401/04 C07D 251/48 C07C 211/40 C07C 233/36 ФЕДЕРАЛЬНАЯ СЛУЖБА C07C 233/46 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07C 311/18 C07D 211/62 C07D 213/12 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 532 545 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D A61K A61K A61K A61P A61P 213/ ...

Patent RU2016136493A3

`”ВУ“” 2016136493” АЗ Дата публикации: 27.07.2018 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение «Федеральный институт промышленной собственности» ж 9 (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2016136493/04(057325) 13.02.2015 РСТ//]Р2015/053979 13.02.2015 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 2014-026617 14.02.2014 ]Р Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ЦИКЛИЧЕСКОЕ УГЛЕВОДОРОДНОЕ СОЕДИНЕНИЕ Заявитель: ТОА ЭЙО ЛТД., ]Р 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты см. п см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 233/41 (2006.01) (070 307/52 (2006.01) Аб1К 31/361 (2006.01) С07С 233/79 (2006.01) (070 333/20 (2006.01) Аб1К 31/40 (2006.01) С07С 247/14 (2006.01) Аб1К 31/165 (2006.01) Аб/1К 31/426 (2006.01) С07С 271/24 (2006.01) Аб1К 31/166 (2006.01) Аб1К 31/655 (2006.01) (070 207/335 (2006.01) Аб/1К 31/27 (2006.01) Аб1Р 9/06 (2006.01) (070 277/28 (2006.01) Аб1К 31/341 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С 233/41, С07С 233/79, СО7С 247/14, СО7С 271/24,СО7О 207/335, С07Ь 277/28, С07Б 307/52, СО7О 333/20, Аб1К 31/165, Аб1К 31/166, ...

ПРОИЗВОДНЫЕ 1,2,3,4-ТЕТРАГИДРО-2-НАФТИЛАМИНА

FIELD: organic chemistry. SUBSTANCE: invention relates to new derivatives of 1,2,3,4-tetrahydro-2-naphthylamine and their pharmaceutically acceptable salts. These compounds show effect on 5-ГТ 1A receptors in mammalian and human and on subclass of dopamine D 2 -receptors and can be used in pharmaceutical industry. EFFECT: enhanced effectiveness of new compounds. 23 cl, 36 tbl

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

... 1. Соединение общей формулы (2) ! ! где Y1, Y1', Y2, Y2', Y3, Y3', Y4 и Y4' в каждом случае независимо друг от друга выбраны из группы, состоящей из -Н, -F, -Cl, -Br, -I, -CN, -NO2, -СНО, -R0, -C(=O)R0, -C(=O)H, -C(=O)-OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -OH, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, -SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NHC(=O)NH2, -NHC(=O)NHR0 и -NHC(=O)N(R0)2; преимущественно в каждом случае независимо друг от друга выбраны из группы, состоящей из -Н, -F, -Cl, -CN и -C1-8-алифат; или Y1 и Y1', или Y2 и Y2', или Y3 и Y3', или Y4 и Y4' совместно означают =O; ! Q означает -R0, -C(=O)-R0, -C(=O)OR0, -C(=O)NHR0, -C(=O)N(R0)2 или -C(=NH)-R0; ! R0 в каждом случае независимо означает -C1-8-алифат, -С3-12-циклоалифат, -арил, -гетероарил, -С1-8-алифат-С3-12-циклоалифат, -C1-8-алифат-арил, -C1-8-алифат-гетероарил, -С3-8-циклоалифат-С1-8-алифат, -С3-8-циклоалифат-арил ...

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

The invention relates to compounds which have an affinity to the µ-opioid receptor and ORL1 receptor, to processes for preparation thereof, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНА

Изобретение относится к новым производным 4-аминоциклогексана, которые обладают сродством к µ-опиоидному рецептору и ORL1-рецептору. В формуле (1) Y 1 , Y 1 ', Y 2 , Y 2 ', Y 3 , Y 3 ', Y 4 и Y 4 ' означают -Н; Q означает -R 0 , -C(=O)-R 0 или -C(=NH)-R 0 ; R 0 и R 3 в каждом случае независимо означает -C 1-8 -алифат, -арил, -гетероарил, -C 1-8 -алифат-С 5 -циклоалифат, -C 1-8 -алифат-арил; R 1 и R 2 , независимо означают незамещенный -C 1-8 -алифат; -C 1-8 -алифат-C 5 -циклоалифат, -C 1-8 -алифат-арил; n означает 0; Х означает -NR A -; R A означает незамещенный -C 1-8 -алифат; R B означает незамещенный -C 1-8 -алифат; «алифат» представляет собой неразветвленный, насыщенный, незамещенный или моно- или многократно замещенный атомами -F углеводородный остаток; «циклоалифат» представляет собой насыщенный, незамещенный моноциклический углеводородный остаток, с 5 атомами углерода в цикле; «арил» означает фенил, который может быть замещенным -F, -R 0 и -OR 0 ; «гетероарил» означает 5-членный циклический ароматический остаток, который содержит 1 гетероатом, причем гетероатом представляет собой N или S, и гетероцикл может быть замещенным -F, -R 0 и -OR 0 ; гетероцикл может быть частью бициклической системы, включающей фенил. Изобретение также относится к лекарственному средству, содержащему указанные соединения, и к применению соединений для получения лекарственного средства для лечения: боли, стресса, эпилепсии, нарушений обучения и памяти, медикаментозной зависимости, сердечно-сосудистых заболеваний, нарушений приема пищи, локомоторных расстройств. 4 н. и 5 з.п. ф-лы, 10 табл., 164 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 503 660 (13) C2 (51) МПК C07D C07C C07D A61K A61K A61K ФЕДЕРАЛЬНАЯ СЛУЖБА A61K ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P A61P A61P (12) ОПИСАНИЕ 209/04 (2006.01) 211/40 (2006.01) 333/10 (2006.01) 31/135 (2006.01) 31/132 (2006.01) 31/381 (2006.01) 31/404 (2006.01) 25/00 (2006.01) 1/00 (2006.01) 9/00 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (72) Автор(ы ...

ЦИКЛИЧЕСКОЕ УГЛЕВОДОРОДНОЕ СОЕДИНЕНИЕ

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2016 136 493 A (51) МПК C07C 233/41 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016136493, 13.02.2015 (71) Заявитель(и): ТОА ЭЙО ЛТД. (JP) Приоритет(ы): (30) Конвенционный приоритет: 14.02.2014 JP 2014-026617 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 14.09.2016 R U (43) Дата публикации заявки: 19.03.2018 Бюл. № 08 (72) Автор(ы): МАСАКИ Хидекадзу (JP), КАГЕЯМА Масаюки (JP) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2015/122494 (20.08.2015) A Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" R U (57) Формула изобретения 1. Соединение, представленное следующей общей формулой (I), его фармацевтически приемлемая соль или его сольват: A 2 0 1 6 1 3 6 4 9 3 (54) ЦИКЛИЧЕСКОЕ УГЛЕВОДОРОДНОЕ СОЕДИНЕНИЕ 2 0 1 6 1 3 6 4 9 3 JP 2015/053979 (13.02.2015) (I) где пунктирная линия обозначает одинарную связь или двойную связь; R1 представляет собой необязательно замещенную С1-6 алкильную группу; Q представляет собой атом кислорода, атом серы или NR5; R5 представляет собой атом водорода, необязательно замещенную C1-6 алкильную группу, или необязательно замещенное неароматическое гетероциклическое кольцо, Стр.: 1 образованное путем объединения с R1 и соседним атомом азота; R2 представляет собой -(C=O)-R6, -CHR6R7 или -CH2OR8; R6 представляет собой необязательно замещенную С1-6 алкильную группу, необязательно замещенную арильную группу или необязательно замещенную гетероарильную группу; R7 представляет собой гидроксильную группу или необязательно замещенную С1-6 алкоксигруппу; R8 представляет собой необязательно замещенную С1-6 алкильную группу; R3 и R4, которые могут быть одинаковыми или различными, каждый представляет собой аминогруппу, азидную группу или -X-R9; R9 представляет собой атом водорода, необязательно замещенную С1-6 алкильную группу, -(C=O)-R10 или -(C=O)-NR11R12; X представляет ...

2-AMINOINDANE ALS SELEKTIVE DOPAMIN-D3-LIGANDEN

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds which have an affinity to the [mu]-opioid receptor and ORL1 receptor, to processes for preparation thereof, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.

NOVEL CYCLOBUTANE DERIVATIVES

Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide

Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5- tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

Therapeutically useful 2-aminotetralin derivatives

NOVEL CYCLOBUTANE DERIVATIVES

Substituted 4-aminocyclohexane derivatives

CRYSTALLINE FORMS OF (S)-5-BENZYL-N-(5-METHYL-4-OXO-2,3,4,5-TETRAHYDROBENZO[B][1,4]OXAZEPIN-3-YL)-4H-1,2,4-TRIAZOLE-3-CARBOXAMIDE

Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5- tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

CYCLOBUTANE DERIVATIVES

Cyclobutane derivatives represented by the formula (1) (1) wherein B is a nucleic acid base derivative, R1 denotes a lower alkyl group of 1 to 6 carbon atoms, and R2 and R3 each independently denote hydrogen atom or a protecting group for hydroxyl, and physiologically acceptable salts thereof. These compounds are expectedly useful as medicinal agents such as antiviral agent, carcinostatic agent and the like.

THERAPEUTICALLY USEFUL 2-AMINOTETRALIN DERIVATIVES

... 2051399 9015047 PCTABS00002 This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of formula (I). These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds which have an affinity to the µ-opioid receptor and ORL1 receptor, to processes for preparation thereof, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.

Substituted 4-aminocyclohexane derivatives

CNS active 8-heterocyclyl-2-aminotetralin derivatives

THERAPEUTICALLY USEFUL 2-AMINOTETRALIN DERIVATIVES

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of formula (I). These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Multi-substituted enamine aldehyde derivative and preparation method thereof

아스코클로린 유도체 및 AMPK 활성제로서의 이의 용도

... 본 발명의 목적은 아데노신 모노포스페이트-활성화 단백질 키나아제 (AMPK) 를 활성화시키고, AMPK 조절장애를 수반하는 질환 또는 병태의 치료 또는 예방에 유용한 신규 아스코클로린 유도체를 제공하는 것이다. 본 발명은 식 I 로 나타나는 화합물, 이의 약학적으로 허용가능한 염 또는 용매화물을 제공한다.

DERIVATIVES OF 4AMINOCICLOHEXANO REPLACED

Compuestos, que poseen afinidad con el receptor de opioides mu y con el receptor ORL-1, a un procedimiento para su obtención, a medicamentos que contienen estos compuestos y al uso de estos compuestos para la fabricación de medicamentos. Reivindicación 1: Compuesto de la fórmula general (1) en la que Y1, Y1', Y2, Y2', Y3, Y3', Y4 e Y4' se eligen en cada caso con independencia entre si entre el grupo formado por -H, -F, -Cl, -Br, -I, -CN, -NO2, -CHO, -R0, -C(=O)R0, -C(=O)H, -C(=O)-OH, -C(=O)OR0, -C(=O)NH2, -C(=O)NHR0, -C(=O)N(R0)2, -OH, -OR0, -OC(=O)H, -OC(=O)R0, -OC(=O)OR0, -OC(=O)NHR0, -OC(=O)N(R0)2, -SH, -SR0, SO3H, -S(=O)1-2-R0, -S(=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(=O)R0, -NHC(=O)OR0, -NH-C(=O)NH2, -NHC(=O)NHR0, -NHC(=O)N(R0)2; con preferencia se eligen en cada caso con independencia entre sí entre el grupo formado por -H, -F, -Cl, -CN y -alifático C1-8; o Y1 e Y1' , o Y2 e Y2', o Y3 e Y3', o Y4 e Y4' juntos significan =O; Q significa -R0, -C(=O)-R0, -C(=O)OR0 ...

Ascochlorin derivative and use thereof as AMPK activator

An object of the present invention is to provide a novel ascochlorin derivative which activates adenosine monophosphate-activated protein kinase (AMPK), and is useful in the treatment or prevention of diseases or conditions that involve AMPK dysregulation. The present invention provides a compound presented by formula I, a pharmaceutically acceptable salt or a solvate thereof.

METHOD OF WHITENING SKIN USING TRANEXAMIC ACID-PEPTIDE HAVING SKIN WHITENING ACTIVITY

A skin whitening method including: administering to a subject a cosmetic composition including a tranexamic acid-peptide having skin whitening activity selected from the group consisting of Tranexamil-AS, Tranexamil-AT, Tranexamil-AP, Tranexamil-GP, Tranexamil-ES, Tranexamil-KK, Tranexamil-HK, Tranexamil-MY, Tranexamil-GH, Tranexamil-MA, Tranexamil-AH, Tranexamil-CC, Tranexamil-SA, Tranexamil-WA, Tranexamil-WE, Tranexamil-KD, Tranexamil-NA, Tranexamil-TS, Tranexamil-SS, Tranexamil-EC, Tranexamil-TA, Tranexamil-PF, Tranexamil-VS, Tranexamil-VV, Tranexamil-VP, Tranexamil-AA, Tranexamil-PS, Tranexamil-HA, Tranexamil-GK, Tranexamil-KV, Tranexamil-AR, Tranexamil-RP, Tranexamil-PQ, Tranexamil-QG, Tranexamil-PP, Tranexamil-VR, Tranexamil-SV, Tranexamil-ET, Tranexamil-CG and Tranexamil-NT.

ZNS-wirksame 8-Heterocyclyl-2-aminotetralin Derivate

Crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide

Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

2-AMINOINDANS AS SELECTIVE DOPAMINE D3 LIGANDS

Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of formula (I), wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CF3, CN, SR5, SO2NH2, SO2NR5R6, SO2R5, -OCO-C1-C6 alkyl, -NCO-C1-C6 alkyl, -CH2O-C1-C6 alkyl, -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-C1-C6 alkyl, phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazol, halogen (Br, Cl, F, I), R6 or R1 and R2 together form -O(CH2)mO- (where m is 1-2) or -CH2(CH2)pCH2 - (where p is 1-4); (except that only one of R1 and R2 can be hydrogen, OCH3 or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p-thienyl (where p is 1-4), hydrogen (except that only one of R3 and R4 can be hydrogen in any such compound) or C1-C8 alkyl (except where R1 or R2 are hydrogen, OCH3 or OH); R5 is hydrogen, C1-C8 ...

THERAPEUTICALLY USEFUL 2-AMINOTETRALIN DERIVATIVES

2-aminoindans as selective dopamine d3 ligands

피부 미백 활성을 가지는 트라넥삼산-펩타이드 및 그 용도

... 피부의 턴오버 개선을 통한 미백 효과 및 건강한 피부로의 회귀를 유도하는 것이 가능하며, 피부 미백효과 및 열적안정성과 시간안정성이 뛰어난 피부 미백 활성을 가지는 트라넥삼산-펩타이드 및 그 용도가 개시된다, 본 발명은 트라넥사밀-AS, 트라넥사밀-AT, 트라넥사밀-AP, 트라넥사밀-GP, 트라넥사밀-ES, 트라넥사밀-KK, 트라넥사밀-HK, 트라넥사밀-MY, 트라넥사밀-GH, 트라넥사밀-MA, 트라넥사밀-AH, 트라넥사밀-CC, 트라넥사밀-SA, 트라넥사밀-WA, 트라넥사밀-WE, 트라넥사밀-KD, 트라넥사밀-NA, 트라넥사밀-TS, 트라넥사밀-SS, 트라넥사밀-EC, 트라넥사밀-TA, 트라넥사밀-PF, 트라넥사밀-VS, 트라넥사밀-VV, 트라넥사밀-VP, 트라넥사밀-AA, 트라넥사밀-PS, 트라넥사밀-HA, 트라넥사밀-GK, 트라넥사밀-KV, 트라넥사밀-AR, 트라넥사밀-RP, 트라넥사밀-PQ, 트라넥사밀-QG, 트라넥사밀-PP, 트라넥사밀-VR, 트라넥사밀-SV, 트라넥사밀-ET, 트라넥사밀-CG 및 트라넥사밀-NT로 구성된 군에서 선택되는 피부 미백 활성을 나타내는 트라넥삼산-펩타이드를 제공한다.

TRANEXAMIC ACID-PEPTIDE HAVING SKIN WHITENING ACTIVITY AND USES THEREOF

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

The invention relates to compounds which have an affinity to the µ-opioid receptor and ORL1 receptor, to processes for preparation thereof, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.

Substituted 4-aminocyclohexane derivatives

Die Erfindung betrifft Verbindungen, welche eine Affinität an den µ-Opioid-Rezeptor und den ORL1-Rezeptor aufweisen, Verfahren zu deren Herstellung, Arzneimittel enthaltend diese Verbindungen und die Verwendung dieser Verbindungen zur Herstellung von Arzneimitteln.

Substituted 4-aminocyclohexane derivatives

Die Erfindung betrifft Verbindungen der vorliegenden Formel (1) welche eine Affinität an den µ-Opioid-Rezeptor und den ORL1-Rezeptor aufweisen, Verfahren zu deren Herstellung, Arzneimittel enthaltend diese Verbindungen und die Verwendung dieser Verbindungen zur Herstellung von Arzneimitteln.

Novel cyclobutane derivatives

Cyclobutane derivatives represented by the formula (1) wherein B is a nucleic acid base derivative, R1 denotes a lower alkyl group of 1 to 6 carbon atoms, and R² and R3 each independently denote hydrogen atom or a protecting group for hydroxyl, and physiologically acceptable salts thereof. These compounds are expectedly useful as medicinal agents such as antiviral agent, carcinostatic agent and the like.

(S)-5-벤질-N-(5-메틸-4-옥소-2,3,4,5-테트라히드로벤조[b][1,4]옥사제핀-3-일)-4H-1,2,4-트리아졸-3-카르복사미드의 결정질 형태

... 신규한 (S)-5-벤질-N-(5-메틸-4-옥소-2,3,4,5-테트라히드로벤조[b][1,4]옥사제핀-3-일)-4H-1,2,4-트리아졸-3-카르복사미드의 결정질 형태, 및 그의 용매화물 및 동일한 것을 함유하는 제약 조성물이 개시된다. 또한 그의 제조 방법 및 그의 사용 방법이 개시된다.

Compuestos derivados de 4-aminociclohexano sustituido; composicion farmaceutica que comprende a dichos compuestos; y su uso como moduladores del receptor de opioides u y el receptor orl-1 en el tratamiento de la ansiedad, estres, depresion, epilepsia y alzheimer.

LA INVENCIÓN SE REFIERE A COMPUESTOS DE FÓRMULA I QUE POSEEN AFINIDAD CON EL RECEPTOR DE OPIOIDES 11 Y CON EL
RECEPTOR ORL-1, A UN PROCEDIMIENTO PARA SU OBTENCIÓN, A MEDICAMENTOS
QUE CONTIENEN ESTOS COMPUESTOS EN FORMA DE ESTEREOISÓMERO INDIVIDUAL
O DE MEZCLA DE VARIOS, DE LOS COMPUESTOS LIBRES Y/O DE SUS SALES
FISIOLÓGICAMENTE COMPATIBLES Y/O SOLVATOS Y AL USO DE ESTOS COMPUESTOS
PARA LA FABRICACIÓN DE MEDICAMENTOS PARA EL TRATAMIENTO DE ESTADOS DE
ANSIEDAD, ESTRÉS, DEPRESIÓN, LA EPILEPSIA, ENFERMEDAD DE ALZHEIMER,
ENTRE OTROS.
...

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

고리형 탄화수소 화합물

... 심방세동을 포함한 부정맥에 대하여, 우수한 억제작용을 가지고, 항바이러스 작용이 분리된 의약품으로써 유용한 신규화합물을 제공한다. 하기 화학식 (I)로 표시되는 화합물, 이의 약학적으로 허용 가능한 염 또는 이들의 용매화물: [화학식 1] 상기 식에서, 점선부는 단일결합, 이중결합을 나타내며; R1은 치환기를 가질 수 있는 C1-6 알킬기를 나타내고; Q는 산소원자, 황원자 또는 NR5를 나타내며; R2는 -(C=O)-R6, -CHR6R7, -CH2OR8을 나타내며; R3, R4는 동일하거나 상이하며, 아미노기, 아지드기 또는 -X-R9을 나타낸다.; 단, R3, R4 중 어느 한쪽은 아미노기이다.

derivados substituídos de 4-aminociclohexano

2-aminoindans as selective dopamine D3 ligands

Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: см. иллюстрацию в PDF-документе wherein R1 and R2 are independently chosen from hydrogen, C1 -C8 alkyl, OCH3, OH, OSO2 CF3, OSO2 CH3, SOR5, CO2 R5, CONH2, CONR5 R6, COR5, CN, SO2 NH2, SO2 NR5 R6, SO2 R5, --OCO--(C1 -C6 alkyl), --NCO--(C1 -C6 alkyl), --CH2 O--(C1 -C6 alkyl), --CH2 OH, --CO-Aryl, --NHSO2 -Aryl, --NHSO2 --(C1 -C6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R1 and R2 together form --O(CH2)1-2 O-- or --(CH2)3-6 -- (except that only one of R1 and R2 can be hydrogen or OH in any such compound); R3 and R4 are independently chosen from C2 -C4 alkenyl, C3 -C8 alkynyl, C3 -C8 cycloalkyl, --(CH2)p -- thienyl (where p is 1-4), or C1 -C8 alkyl (except where R1 or R2 are hydrogen or OH or where both R1 and R2 are OCH3 or a C1 -C8 alkyl); R5 is hydrogen, C1 -C8 alkyl, C2 -C4 alkenyl, C3 -C8 cycloalkyl ...

2-AMINOINDANE ALS SELEKTIVE DOPAMIN-D3-LIGANDEN

ZNS-wirksame 8-Heterocyclyl-2-aminotetralin Derivate

CYELOBUTANE DERIVATIVES

Substituted 4-aminocyclohexane derivatives

compostos derivados substituídos de 4-aminociclohexano, composição farmacêutica e uso dos referidos compostos

Therapeutically useful 2-aminotetralin derivatives

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formulaThese compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

composto de hidrocarboneto cíclico

TRANEXAMIC ACID-PEPTIDE HAVING SKIN WHITENING ACTIVITY AND USE THEREOF

Disclosed are a tranexamic acid-peptide having skin whitening activity, which has a whitening effect through skin turnover improvement, is capable of inducing return to health skin, and exhibits a skin whitening effect and excellent thermal stability and time stability, and a use thereof. The tranexamic acid-peptide having skin whitening activity is selected from the group consisting of Tranexamil-AS, Tranexamil-AT, Tranexamil-AP, Tranexamil-GP, Tranexamil-ES, Tranexamil-KK, Tranexamil-HK, Tranexamil-MY, Tranexamil-GH, Tranexamil-MA, Tranexamil-AH, Tranexamil-CC, Tranexamil-SA, Tranexamil-WA, Tranexamil-WE, Tranexamil-KD, Tranexamil-NA, Tranexamil-TS, Tranexamil-SS, Tranexamil-EC, Tranexamil-TA, Tranexamil-PF, Tranexamil-VS, Tranexamil-VV, Tranexamil-VP, Tranexamil-AA, Tranexamil-PS, Tranexamil-HA, Tranexamil-GK, Tranexamil-KV, Tranexamil-AR, Tranexamil-RP, Tranexamil-PQ, Tranexamil-QG, Tranexamil-PP, Tranexamil-VR, Tranexamil-SV, Tranexamil-ET, Tranexamil-CG and Tranexamil-NT. COPYRIGHT ...

Ascochlorin derivative and use thereof as AMPK activator

An object of the present invention is to provide a novel ascochlorin derivative which activates adenosine monophosphate-activated protein kinase (AMPK), and is useful in the treatment or prevention of diseases or conditions that involve AMPK dysregulation. The present invention provides a compound presented by formula I, a pharmaceutically acceptable salt or a solvate thereof.

2-aminoindans as selective dopamine D3 ligands

PCT No. PCT/US94/08046 Sec. 371 Date May 14, 1996 Sec. 102(e) Date May 14, 1996 PCT Filed Jul. 21, 1994 PCT Pub. No. WO95/04713 PCT Pub. Date Feb. 16, 1995Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CN, SO2NH2, SO2NR5R6, SO2R5, -OCO-(C1-C6 alkyl), -NCO-(C1-C6 alkyl), -CH2O-(C1-C6 alkyl), -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-(C1-C6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R1 and R2 together form -O(CH2)1-2O- or -(CH2)3-6- (except that only one of R1 and R2 can be hydrogen or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p- thienyl (where p is 1-4), or C1-C8 alkyl (except where R1 or R2 are hydrogen or OH or where both R1 and ...

Substituted 4-aminocyclohexane derivatives

The invention relates to compounds which have an affinity to the [mu]-opioid receptor and ORL1 receptor, to processes for preparation thereof, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.

Therapeutically useful 2-aminotetralin derivatives

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula I R, R1 to R5 and p are as defined in the specification, these compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

THERAPEUTICALLY USEFUL 2-AMINOTETRALIN DERIVATIVES

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of formula (I). These compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

置換された４−アミノシクロヘキサン誘導体

2-AMINOINDANS AS SELECTIVE DOPAMINE D3 LIGANDS

置換された４−アミノシクロヘキサン誘導体

formas cristalinas de (s)-5-benzil-n-(5-metil-4-oxo-2,3,4,5-tetraidrobenzo[b][1,4]oxazepin-3-il)-4h-1,2,4-triazol-3-carboxamida

Cyclic hydrocarbon compound

本发明提供一种对包括心房颤动在内的心律不齐具有优异的抑制作用、抗病毒作用被分离的作为医药品有用的新型化合物。下述的通式(I)表示的化合物、其药学上允许的盐或者它们的溶剂合物。 式中，虚线部分表示单键，双键；R 1 表示可以具有取代基的C 1-6 烷基；Q表示氧原子、硫原子或者NR 5 ；R 2 表示-(C＝O)-R 6 、-CHR 6 R 7 、-CH 2 OR 8 ；R 3 、R 4 相同或不同，表示氨基、叠氮基或者-X-R 9 ；其中，R 3 、R 4 中的任一者为氨基。

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

The invention relates to compounds that have an affinity to the mu-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

HIGHLY ENANTIOSELECTIVE ACCESS TO CYCLIC BETA-AMINO ACIDS

Disclosed herein is a method of forming a compound of formula I: 2. The method according to claim 1 , wherein Rand Reach independently represent ROC(O)— claim 1 , Cto Calkyl claim 1 , phenyl claim 1 , and naphthyl claim 1 , where the Cto Calkyl claim 1 , phenyl claim 1 , and naphthyl are unsubstituted or substituted by one or more substituents selected from the group consisting of halo and Cto Calkyl claim 1 , which Cto Calkyl is unsubstituted or substituted by one or more halo groups.3. The method according to claim 1 , wherein Rrepresents H claim 1 , Cto Calkyl claim 1 , and phenyl claim 1 , where the Cto Calkyl and phenyl are unsubstituted or substituted by one or more substituents selected from the group consisting of halo and Cto Calkyl claim 1 , which Cto Calkyl is unsubstituted or substituted by one or more halo groups.4. The method according to claim 1 , wherein Rrepresents Cto Calkyl claim 1 , Cto Calkenyl claim 1 , phenyl claim 1 , naphthyl and furanyl claim 1 , where the Cto Calkyl claim 1 , Cto Calkenyl claim 1 , phenyl claim 1 , naphthyl and furanyl are unsubstituted or substituted by one or more substituents selected from the group consisting of halo claim 1 , phenyl claim 1 , OCto Calkyl and Cto Calkyl claim 1 , which phenyl claim 1 , OCto Calkyl and Cto Calkyl are unsubstituted or substituted by one or more halo groups.5. The method according to claim 1 , wherein Ris selected from a tosyl group claim 1 , a nosyl group claim 1 , and a diphenylphosphinyl group and suitable isomers thereof.6. The method according to claim 1 , wherein Rand Rand Rto Rare each independently Cto Calkyl that is unsubstituted or substituted by one or more halo groups.8. The method according to claim 1 , wherein the base further comprises a further base selected from one or more of the group consisting of KHPO claim 1 , an amine base claim 1 , and NaHPO.9. The method according to claim 8 , wherein the amine base is selected from one or more of the group consisting of EtN claim ...

Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide

Method of whitening skin using tranexamic acid-peptide having skin whitening activity

A skin whitening method including: administering to a subject a cosmetic composition including a tranexamic acid-peptide having skin whitening activity selected from the group consisting of Tranexamil-AS, Tranexamil-AT, Tranexamil-AP, Tranexamil-GP, Tranexamil-ES, Tranexamil-KK, Tranexamil-HK, Tranexamil-MY, Tranexamil-GH, Tranexamil-MA, Tranexamil-AH, Tranexamil-CC, Tranexamil-SA, Tranexamil-WA, Tranexamil-WE, Tranexamil-KD, Tranexamil-NA, Tranexamil-TS, Tranexamil-SS, Tranexamil-EC, Tranexamil-TA, Tranexamil-PF, Tranexamil-VS, Tranexamil-VV, Tranexamil-VP, Tranexamil-AA, Tranexamil-PS, Tranexamil-HA, Tranexamil-GK, Tranexamil-KV, Tranexamil-AR, Tranexamil-RP, Tranexamil-PQ, Tranexamil-QG, Tranexamil-PP, Tranexamil-VR, Tranexamil-SV, Tranexamil-ET, Tranexamil-CG and Tranexamil-NT.

置換された4-アミノシクロヘキサン誘導体

... 本発明は、μ-オピオイド受容体およびORL1受容体への親和性を示す化合物、その製造方法、この化合物を含有する医薬ならびに医薬製造へのこの化合物の使用に関する。 ...

ASCOCHLORIN DERIVATIVE AND USE THEREOF AS AMPK ACTIVATOR

An object of the present invention is to provide a novel ascochlorin derivative which activates adenosine monophosphate-activated protein kinase (AMPK), and is useful in the treatment or prevention of diseases or conditions that involve AMPK dysregulation. The present invention provides a compound presented by formula I, a pharmaceutically acceptable salt or a solvate thereof.

Substituted 4-aminocyclohexane derivatives

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

The invention relates to compounds that have an affinity to the μ-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

SUBSTITUTED 4-AMINOCYCLOHEXANE DERIVATIVES

The invention relates to compounds that have an affinity to the -opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.

CYCLIC HYDROCARBON COMPOUND

Provided is a novel compound having an excellent suppression effect against arrhythmia including atrial fibrillation and being useful as a pharmaceutical product without antiviral effect. Disclosed is a compound represented by the following General Formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof (in the formula, the dotted line portion represents a single bond or a double bond; Rrepresents an optionally substituted Calkyl group; Q represents an oxygen atom, a sulfur atom, or NR; Rrepresents —(C═O)—R, —CHRR, or —CHOR; and Rand R, which may be identical or different, each represent an amino group, an azide group, or —X—R, with the proviso that any one of Rand Ris an amino group). 2: The compound according to claim 1 , a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , wherein the dotted line portion in Formula (I) represents a double bond.4: The compound according to claim 1 , a pharmaceutically acceptable salt thereof claim 1 , or a solvate thereof claim 1 , wherein the substituent which the Calkyl group claim 1 , the aryl group claim 1 , the heteroaryl group claim 1 , the Calkoxy group claim 1 , or the non-aromatic heterocyclic ring has is one to five substituents selected from the group consisting of a halogen atom claim 1 , a hydroxyl group claim 1 , a cyano group claim 1 , a nitro group claim 1 , a Calkyl group claim 1 , a Calkenyl group claim 1 , a Calkoxy group claim 1 , an acyl group claim 1 , a carboxyl group claim 1 , a Calkylcarbonylamino group claim 1 , a Calkoxycarbonyl group claim 1 , a carbamoyl group claim 1 , a sulfamoyl group claim 1 , a Calkylsulfanyl group claim 1 , a Calkylsulfenyl group claim 1 , a Calkylsulfonyl group claim 1 , an amino group claim 1 , a Calkylamino group claim 1 , a Cdialkylamino group claim 1 , an aryl group claim 1 , a heteroaryl group claim 1 , and a non-aromatic heterocyclic ring group.5: The compound according to claim 1 , a pharmaceutically acceptable salt ...

ASCOCHLORIN DERIVATIVE AND USE THEREOF AS AMPK ACTIVATOR

Therapeutically useful 2-aminotetralin derivatives

This invention is therapeutically useful 2-aminotetralins and pharmaceutically acceptable acid addition salts thereof of the formula см. иллюстрацию в PDF-документе R, R1 to R5 and p are as defined in the specification, these compounds are useful to treat central nervous system disorders, hypertension, diabetes, sexual impotency and to control appetite.

Cyclic hydrocarbon compound

Provided is a novel compound having an excellent suppression effect against arrhythmia including atrial fibrillation and being useful as a pharmaceutical product without antiviral effect. Disclosed is a compound represented by the following General Formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof (in the formula, the dotted line portion represents a single bond or a double bond; R 1 represents an optionally substituted C 1-6 alkyl group; Q represents an oxygen atom, a sulfur atom, or NR 5 ; R 2 represents —(C═O)—R 6 , —CHR 6 R 7 , or —CH 2 OR 8 ; and R 3 and R 4 , which may be identical or different, each represent an amino group, an azide group, or —X—R 9 , with the proviso that any one of R 3 and R 4 is an amino group).

CRYSTALLINE FORMS OF (S)-5-BENZYL-N-(5-METHYL-4-OXO-2,3,4,5-TETRAHYDROBENZO[b][1,4]OXAZEPIN-3-YL)-4H-1,2,4-TRIAZOLE-3-CARBOXAMIDE

Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof. 2. The crystalline form according to claim 1 , wherein claim 1 , the crystalline form is a pharmaceutically acceptable crystalline form.3. The crystalline form according to claim 1 , wherein the solvate is a methyl acetate solvate claim 1 , and wherein the crystalline form is characterized by an X-ray powder diffraction pattern substantially in accordance with .4. The crystalline form according to claim 1 , wherein the solvate is a methyl acetate solvate claim 1 , and wherein the crystalline form is characterized by diffraction data substantially in accordance with Table 2.56-. (canceled)7. The crystalline form according to claim 1 , wherein the solvate is an n-propyl acetate solvate claim 1 , and wherein the crystalline form is characterized by an X-ray powder diffraction pattern substantially in accordance with .8. The crystalline form according to claim 1 , wherein the solvate is an n-propyl acetate solvate claim 1 , and wherein the crystalline form is characterized by diffraction data substantially in accordance with Table 4.9. The crystalline form according to claim 1 , wherein the solvate is an isopropyl acetate solvate claim 1 , and wherein the crystalline form is characterized by an X-ray powder diffraction pattern substantially in accordance with .10. The crystalline form according to claim 1 , wherein the solvate is an isopropyl acetate solvate claim 1 , and wherein the crystalline form is characterized by diffraction data substantially in accordance with Table 5.11. The crystalline form according to claim 1 , wherein the solvate is an ethanol solvate claim 1 , and wherein the crystalline form is characterized by an X-ray powder diffraction pattern ...

环状烃化合物

本发明提供一种对包括心房颤动在内的心律不齐具有优异的抑制作用、抗病毒作用被分离的作为医药品有用的新型化合物。下述的通式(I)表示的化合物、其药学上允许的盐或者它们的溶剂合物。 式中，虚线部分表示单键，双键；R 1 表示可以具有取代基的C 1‑6 烷基；Q表示氧原子、硫原子或者NR 5 ；R 2 表示‑(C＝O)‑R 6 、‑CHR 6 R 7 、‑CH 2 OR 8 ；R 3 、R 4 相同或不同，表示氨基、叠氮基或者‑X‑R 9 ；其中，R 3 、R 4 中的任一者为氨基。

Cyclic hydrocarbon compound

Substituted 4-aminocyclohexane derivatives

Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide

Disclosed are novel crystalline forms of (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5- tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide, and solvates thereof and pharmaceutical compositions containing the same. Also disclosed are processes for the preparation thereof and methods for use thereof.

THERAPEUTIC ANVAENDBARA 2-AMINOTETRAL DERIVATIVES.

Substituted 4-aminocyclohexane derivatives, medicaments comprising the same and use of the compounds in the manufacture of medicaments for treating pain

Ascochylomycete derivatives and their use as AMPK activators

本发明的一个目的是提供一种新型壳二孢氯素(ascochlorin)衍生物，其激活单磷酸腺苷激活的蛋白激酶(AMPK)，并且可用于治疗或预防涉及AMPK失调的疾病或病况。本发明提供了由式I表示的化合物、其药学上可接受的盐或溶剂合物。

2-aminoindans as selective dopamine d3 ligands

Substituted 4-aminocyclohexane derivatives

Compuesto de fórmula general (2.2) **(Ver fórmula)** donde Q representa arilo o heteroarilo; R1 representa -CH3; R2 representa -H o -CH3; o R1 y R2 juntos forman un anillo y representan -(CH2)3-4; X representa NRA-; RA representa -H o un grupo alifático(C1-8); v RB representa -C>=O-alifático(C1-8) o -C>=O-alifático(C1-8)-heteroarilo; RC representa -H, -F, -Cl, -Br, -I, -CN, -NO2, -CF3, -OH u -OCH3, y n representa 0, donde el alifático, arilo o heteroarilo en cada caso está no sustituido o mono o polisustituido; "alifático" es en cada caso un grupo hidrocarburo alifático lineal o ramificado, saturado o mono- o poliinsaturado, no sustituido o sustituido una o más veces; "cicloalifático" es en cada caso un grupo hidrocarburo alicíclico, mono- o policíclico, saturado o mono- o poliinsaturado, no sustituido o sustituido una o varias veces, donde el número de átomos de carbono del anillo preferentemente está en el intervalo indicado (es decir, cicloalifático "C3-8" indica preferentemente 3, 4, 5, 6, 7 u 8 átomos de carbono de anillo); pudiendo sustituirse en cada caso uno o más átomos de carbono por un heteroátomo seleccionado de S, N u O; en lo referente a "alifático" y "cicloalifático" se entiende por "sustituido una o varias veces" la sustitución única o múltiple de uno o varios átomos de hidrógeno, por ejemplo la sustitución una vez, dos veces, tres veces o total, por sustituyentes seleccionados independientemente entre sí de entre el grupo formado por -F, -Cl, -Br, -I, -CN, -NO2, -CHO, >=O, -R0, -C(>=O)R0, -C(>=O)H, -C(>=O)OH, -C(>=O)OR0, -C(>=O)NH2, -C(>=O)NHR0, -C(>=O)N(R0)2, -OH, -OR0, -OC(>=O)H, -OC(>=O)R0, -OC(>=O)OR0, -OC(>=O)NHR0, -OC(>=O)N(R0)2, -SH, -SR0, -SO3H, -S(>=O)1-2-R0, -S(>=O)1-2NH2, -NH2, -NHR0, -N(R0)2, -N+(R0)3, -N+(R0)2O-, -NHC(>=O)R0, -NHC(>=O)OR0, -NHC(>=O)NH2, -NHC(>=O)-NHR0, -NH-C(>=O)N(R0)2, -Si(R0)3 y -PO(OR0)2, donde R0 ...

2-Aminoindanes as selective dopamine D3 ligands

PCT No. PCT/US94/08046 Sec. 371 Date May 14, 1996 Sec. 102(e) Date May 14, 1996 PCT Filed Jul. 21, 1994 PCT Pub. No. WO95/04713 PCT Pub. Date Feb. 16, 1995Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: <IMAGE> wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CN, SO2NH2, SO2NR5R6, SO2R5, -OCO-(C1-C6 alkyl), -NCO-(C1-C6 alkyl), -CH2O-(C1-C6 alkyl), -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-(C1-C6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R1 and R2 together form -O(CH2)1-2O- or -(CH2)3-6- (except that only one of R1 and R2 can be hydrogen or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p- thienyl (where p is 1-4), or C1-C8 alkyl (except where R1 or R2 are hydrogen or OH or where both R1 and R2 are OCH3 or a C1-C8 alkyl); R5 is hydrogen, C1-C8 alkyl, C2-C4 alkenyl, C3-C8 cycloalkyl; and R6 is C1-C8 alkyl, C2-C4 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, or Aryl.

2-AMINOINDANES AS SELECTIVE D3 LIGANDS OF DOPAMINE.

PCT No. PCT/US94/08046 Sec. 371 Date May 14, 1996 Sec. 102(e) Date May 14, 1996 PCT Filed Jul. 21, 1994 PCT Pub. No. WO95/04713 PCT Pub. Date Feb. 16, 1995Compounds and their pharmaceutically acceptable salts suitable for treating central nervous system disorders associated with the dopamine D3 receptor activity of Formula I: <IMAGE> wherein R1 and R2 are independently chosen from hydrogen, C1-C8 alkyl, OCH3, OH, OSO2CF3, OSO2CH3, SOR5, CO2R5, CONH2, CONR5R6, COR5, CN, SO2NH2, SO2NR5R6, SO2R5, -OCO-(C1-C6 alkyl), -NCO-(C1-C6 alkyl), -CH2O-(C1-C6 alkyl), -CH2OH, -CO-Aryl, -NHSO2-Aryl, -NHSO2-(C1-C6 alkyl), phthalimide, thiophenyl, pyrrol, pyrrolinyl, oxazolyl, or R1 and R2 together form -O(CH2)1-2O- or -(CH2)3-6- (except that only one of R1 and R2 can be hydrogen or OH in any such compound); R3 and R4 are independently chosen from C2-C4 alkenyl, C3-C8 alkynyl, C3-C8 cycloalkyl, -(CH2)p- thienyl (where p is 1-4), or C1-C8 alkyl (except where R1 or R2 are hydrogen or OH or where both R1 and R2 are OCH3 or a C1-C8 alkyl); R5 is hydrogen, C1-C8 alkyl, C2-C4 alkenyl, C3-C8 cycloalkyl; and R6 is C1-C8 alkyl, C2-C4 alkenyl, C2-C8 alkynyl, C3-C8 cycloalkyl, or Aryl.

2-aminoindane als selektive dopamin-d3-liganden

联苯类化合物、其制备方法及应用

本发明涉及一种式(I)所示联苯类化合物、其制备方法及其应用。本发明还涉及包含所述化合物作为活性成分的药物组合物。所述化合物是小分子免疫调节剂，可用于治疗和/或预防与免疫相关的多种疾病。

具有皮肤美白活性的凝血酸-肽及其用途

本发明公开了一种具有皮肤美白效果和皮肤美白活性的具有优异的热稳定性和时间稳定性的凝血酸‑肽，其能够通过皮肤更新改善而诱导恢复健康的皮肤和美白效果，及其用途。本发明提供了一种具有皮肤美白活性的凝血酸‑肽，其选自由以下项组成的组：Tranexamil‑AS、Tranexamil‑AT、Tranexamil‑AP、Tranexamil‑GP、Tranexamil‑ES、Tranexamil‑KK、Tranexamil‑HK、Tranexamil‑MY、Tranexamil‑GH、Tranexamil‑MA、Tranexamil‑AH、Tranexamil‑CC、Tranexamil‑SA、Tranexamil‑WA、Tranexamil‑WE、Tranexamil‑KD、Tranexamil‑NA、Tranexamil‑TS、Tranexamil‑SS、Tranexamil‑EC、Tranexamil‑TA、Tranexamil‑PF、Tranexamil‑VS、Tranexamil‑VV、Tranexamil‑VP、Tranexamil‑AA、Tranexamil‑PS、Tranexamil‑HA、Tranexamil‑GK、Tranexamil‑KV、Tranexamil‑AR、Tranexamil‑RP、Tranexamil‑PQ、Tranexamil‑QG、Tranexamil‑PP、Tranexamil‑VR、Tranexamil‑SV、Tranexamil‑ET、Tranexamil‑CG和Tranexamil‑NT。

피부 미백 활성을 가지는 트라넥삼산-펩타이드 및 그 용도

피부의 턴오버 개선을 통한 미백 효과 및 건강한 피부로의 회귀를 유도하는 것이 가능하며, 피부 미백효과 및 열적안정성과 시간안정성이 뛰어난 피부 미백 활성을 가지는 트라넥삼산-펩타이드 및 그 용도가 개시된다, 본 발명은 트라넥사밀-AS, 트라넥사밀-AT, 트라넥사밀-AP, 트라넥사밀-GP, 트라넥사밀-ES, 트라넥사밀-KK, 트라넥사밀-HK, 트라넥사밀-MY, 트라넥사밀-GH, 트라넥사밀-MA, 트라넥사밀-AH, 트라넥사밀-CC, 트라넥사밀-SA, 트라넥사밀-WA, 트라넥사밀-WE, 트라넥사밀-KD, 트라넥사밀-NA, 트라넥사밀-TS, 트라넥사밀-SS, 트라넥사밀-EC, 트라넥사밀-TA, 트라넥사밀-PF, 트라넥사밀-VS, 트라넥사밀-VV, 트라넥사밀-VP, 트라넥사밀-AA, 트라넥사밀-PS, 트라넥사밀-HA, 트라넥사밀-GK, 트라넥사밀-KV, 트라넥사밀-AR, 트라넥사밀-RP, 트라넥사밀-PQ, 트라넥사밀-QG, 트라넥사밀-PP, 트라넥사밀-VR, 트라넥사밀-SV, 트라넥사밀-ET, 트라넥사밀-CG 및 트라넥사밀-NT로 구성된 군 에서 선택되는 피부 미백 활성을 나타내는 트라넥삼산-펩타이드를 제공한다.

New cyclobutane derivatives and process for their production

신규 시클로부탄 유도체

내용 없음

Zns-wirksame 8-heterocyclyl-2-aminotetralin derivate

联苯类化合物、其制备方法及应用

本发明涉及一种式(I)所示联苯类化合物、其制备方法及其应用。本发明还涉及包含所述化合物作为活性成分的药物组合物。所述化合物是小分子免疫调节剂，可用于治疗和/或预防与免疫相关的多种疾病。

具有皮肤美白活性的凝血酸-肽及其用途

本发明公开了一种具有皮肤美白效果和皮肤美白活性的具有优异的热稳定性和时间稳定性的凝血酸‑肽，其能够通过皮肤更新改善而诱导恢复健康的皮肤和美白效果，及其用途。本发明提供了一种具有皮肤美白活性的凝血酸‑肽，其选自由以下项组成的组：Tranexamil‑AS、Tranexamil‑AT、Tranexamil‑AP、Tranexamil‑GP、Tranexamil‑ES、Tranexamil‑KK、Tranexamil‑HK、Tranexamil‑MY、Tranexamil‑GH、Tranexamil‑MA、Tranexamil‑AH、Tranexamil‑CC、Tranexamil‑SA、Tranexamil‑WA、Tranexamil‑WE、Tranexamil‑KD、Tranexamil‑NA、Tranexamil‑TS、Tranexamil‑SS、Tranexamil‑EC、Tranexamil‑TA、Tranexamil‑PF、Tranexamil‑VS、Tranexamil‑VV、Tranexamil‑VP、Tranexamil‑AA、Tranexamil‑PS、Tranexamil‑HA、Tranexamil‑GK、Tranexamil‑KV、Tranexamil‑AR、Tranexamil‑RP、Tranexamil‑PQ、Tranexamil‑QG、Tranexamil‑PP、Tranexamil‑VR、Tranexamil‑SV、Tranexamil‑ET、Tranexamil‑CG和Tranexamil‑NT。

多取代烯胺醛衍生物及其制备方法

本发明提供了一种多取代烯胺醛衍生物及其制备方法，包括：将丙烯醛或丙烯醛衍生物、叠氮化合物或叠氮衍生物、强酸和溶剂置于反应容器中，在0℃以下反应10～60min，再加入甲醇，继续反应10～120min，反应完成后加入三乙胺终止反应；将反应液用二氯甲烷稀释，再经水洗，得有机相；其中，二氯甲烷的用量是所述溶剂体积的5～10倍；将得到的有机相经干燥、浓缩和柱层析纯化，得到多取代烯胺醛衍生物；所述多取代烯胺醛衍生物的结构式如下：